REFERAT

VAKSIN KOKAIN
 Introduction
UNODC
- Worldwide estimates between 0.3% - 0.4%
- Adult population between 15–19 million
- The highest prevalence of cocaine use remains in
North America
- Cocaine addiction is a major social and medical
problem for which there is no effective therapy
- Anti-Cocaine Vaccine as a candidate to treat and
prevent cocaine dependence
 Definition
Immunotherapeutic approach to
treating cocaine dependence which
induces the immune system to form
antibodies that prevent cocaine
from crossing the blood brain
barrier to act on receptor sites in the
brain.
Cocaine vaccine reserch status
 Types of cocaine vaccine candidate

- TA-CD (anti-cocaine Vaccine)

- GND-KLH (Second-generation cocaine
immunoconjugate GND-keyhole limpet
hemocyanin)
- Catalytic antibodies
- COC-AB
 TA-CD (anti-cocaine Vaccine)
- TA-CD is a therapeutic cocaine vaccine
composed of Succinylnorcocaine coupled to an
inactive recombinant cholera toxin B carrier
protein.
- Active immunisation
- Use in relapse prevention and is not effective
in overdose
 TA-CD (anti-cocaine Vaccine)
In the phase I trial:
- The outpatient trial comparing low to high dose
vaccination (100 mcg Inj.4x,or 400 mcg inj. 5x)
→ less relapse with the high dose (89% vs
43%).
- Adverse effects : mild tachycardia, elevated
temperatureor, hypertension
 TA-CD (anti-cocaine Vaccine)
The phase II trial:
- Gave 360 mg for five injections and about one-
third attained antibody levels above 43 mg/ml
- This high antibody group had more cocaine
free urines than the low antibody
- Boosting with this conjugate vaccine is
required about every 3 months to maintain
high antibody levels.
 TA-CD (anti-cocaine Vaccine)

Phase IIb clinical trial:

- Multi-site (double-blind, randomized, placebo-
controlled, multicentre study includes)→
Ongoing
 GND-KLH
Vaccination type and mechanism
- Consists of a modified cocaine derivative
conjugated with keyhole limpet haemocyanin
(KLH).
- The availability of both active and passive
immunisation.
 15 A 10 (Catalytic antibodies)
Vaccination type and mechanism

- Catalytic antibodies have been modelled on

the cocaine-metabolising properties of the
human enzyme butyrylcholinesterase (BChE).
- Destabilise cocaine molecules→break down
into non-toxic or nonpsychoactive fragments.
 COC-AB
Vaccination type and mechanism:
- The vaccine antibodies attach to free cocaine
in the blood and act as an osmotic pump
drawing cocaine out of the brain, heart,
muscles and tissues.
- May be best for overdose
Cocaine in the brain
Antibody actions in blocking
abused drugs
Antibody actions in blocking
abused drugs
 summary
- Cocaine addiction is a serious problem in
worldwide
- There are no currentiy no single
pharmacotherapies to help addict to quit
- TA-CD is a novel approach to treatment,
targeting cocaine in circulation
- Proof of concept established in preclinical
studies
- Phase I,II have shown : vaccine is safe and well
tolerate, promising indications of efficacy